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42 Cards in this Set

  • Front
  • Back

Why are anti psychotic drugs called major tranquilizers

They calm the nerves

What is the major cause of psychosis

Over firing of the dopaminergic neurones


MOA of antipsychotics

They block the dopaminergic receptors especially D2 receptors

Types of symptoms of psychosis

1) positive symptoms


2) negative symptoms

Positive symptoms of psychosis

1) delusion


2) wild thoughts/ wild imagination


3) hallucinations


4) aggressive behaviour


5) irrational conclusion

Negative symptoms of psychosis

1) apathy


2) withdrawal from social life


3) avolition( lack of motivation)


4) cognitive deficits

Theories that explain psychosis

1) dopamine theory


2) glutamate theory

Dopamine theory

Psychosis is as a result of excess of dopaminergic activity

Facts that support the dopamine theory

1) postmortem studies on the brain of schizophrenic patients who were not treated with anti-psychotic drugs showed increase in dopaminergic receptors


2) drugs that increase dopaminergic activity like laevodopa worsen schizophrenia


3) there is a decrease in the dopamine metabolite called homovanilic acid when the patient takes antipsychotic drugs

Glutamate theory

Glutamate is the major "excitatory" neurotransmitter in the brain, which means that it helps to activate neurons and other brain cells.The multiple areas of the brain involved in schizophrenia are connected by a circuit of brain cells that rely on glutamate to communicate. Research so far suggests that either excess or insufficient glutamate activity may cause symptoms, partly through its interactions with other neurotransmitters like dopamine and gamma-aminobutyric acid (GABA).


Glutamatergic models are based upon the observation that the psychotomimetic agents such as phencyclidine (PCP) and ketamine induce psychotic symptoms and neurocognitive disturbances similar to those of schizophrenia by blocking neurotransmission at N-methyl-D-aspartate (NMDA)-type glutamate receptors. Because glutamate/NMDA receptors are located throughout the brain, glutamatergic models predict widespread cortical dysfunction with particular involvement of NMDA receptors throughout the brain. Further, NMDA receptors are located on brain circuits that regulate dopamine release, suggesting that dopaminergic deficits in schizophrenia may also be secondary to underlying glutamatergic dysfunction.

Classification of antipsychotics

1) first generation/ typical antipsychotics


2) second generation/ atypical antipsychotics

What criteria is used to classify antipsychotics

Their selectivity to dopamine receptors

Disadvantages of the Typicals

1) they have severe side effects


2) they are used in combination with the second generation because when used alone, they have resistance issues

Why are the typicals considered as the best bet for treatment

They are more potent than the atypicals

Classification of the Typical antipsychotics

1) phenothiazones


2) thioxanthines


3) butyrophenones



Phyno is TIRED of his BOOTS and PHYNO is TIRED of his XANS

Classification of the phenothiazones

Aliphatics and piperidines

Examples of aliphatic phenothiazones

1) chloropromazine


2) triflupromazine


think of CHLOROQUINE and The FLU and PROMAC PHARMACY

Examples of piperidines phenothiazones

Mesoridazine

Classification of the thioxanthines

Aliphatics and piperidines

Example of aliphatic thioxanthines

Chlorprothixene

Example of piperidine thioxanthine

Flupenthixol

Examples of butyrophenones

Haloperidol and Droperidol

What class of drugs do the Atypicals belong to

Dibenzodiazepines

Classification of the dopamine receptors

D1-like : D1 and D5 receptors


D2-like : D2, D3 and D4 receptors

Dopaminergic pathways in the brain

1) nigrostatial pathway


2) mesolimbic-mesocortical pathway


3) tuberoinfundibular pathway


Significance of the nigrostatial pathway

It deals with voluntary movement and posture. Blockade of this pathway leads to extrapyramidal side effects

Significance of mesolimbic-mesocortical pathway

Higher mental and emotional function. Overfiring results in psychosis. The major role of anti-psychotic drugs lies in this pathway

Significance of the tuberoinfundibular pathway

Activation of this pathway inhibits prolactin secretion i.e milk secretion

Diseases where antipsychotics are used

1) schizophrenia


2) tourrette syndrome


3) nausea and vomitting


4) mania disorders


5) Alzheimer's


6) Huntington's disease

Pharmacological actions of anti-psychotic drugs

1)CNS depressants


2) decrease seizure threshold ( it worsens seizure); it is not taken alongside anti-seizure drugs


3) weight gain ( especially the Atypicals)


4) orthostatic hypotension


5) decreased libido in women; amenorrhea and infertility


6) decreased libido in men; gynaecomastia


7) serious neurological effects/extrapyramidal side effects (EPS)-akatisia, dyskenisia, Parkinsonism, dystonia and tremor and neuroleptic malignant syndrome


8) as antiemetics e.g promethazine

What is akathisia

A sensation of restlessness characterized by an inability to sit still/down or remain motionless/seated, arising from a subjective need or desire to move, often coinciding with the sensation of twitching of muscles, often as a side effect of psychiatric medications.

Drugs that can be used to treat akathisia

1) benzodiazepines


2) non-selective beta blockers

What is dystonia

Uncontrolled movements of the head, neck, face and tongue

Drugs used to control distonia

Centrally acting anti-muscarinic agents e.g benztropine

What is parkinsonism

A neurological syndrome characterized by tremor, bradykinesia, rigidity, and postural instability;

Symptoms of neuroleptic malignant syndrome

Fever


Increased blood pressure


Extreme rigidity


Increased heart rate

Drug used in neuroleptic malignant syndrome

Bromocriptine and dantrolene

What is dyskinesia

impairment of voluntary movements resulting in fragmented or jerky motions

How to manage dyskinesia

Discontinue the antipsychotic. Replace

Other side effects of antipsychotics

1) gynaecomastia


2) amenorrhea


3) breast engorgement


4) infertility


5) weight gain


6) cholesteric jaundice caused by chlorpromazine


7) glycopenia


8) blurred vision


9) retinopathy

Contraindications of antipsychotics

1) hypotension


2) CNS depression


3) Parkinsons


4) bone marrow depression


5) hepatic failure because they are metabolized by cytochrome P450


6) seizure

Drug interactions of anti-psychotics

1) inhibit action of dopamine and laevodopa


2) concomitant administration with diuretics and antihypertensives lead to marked hypotensive effect


Give a 2-3hr interval between drugs